Vps34-IN-5
Vps34-IN-5 is an orally active VPS34 inhibitor, 98% target inhibition, and an IC50 categorized as B. Vps34-IN-5 induces additive or synergistic anti-proliferative activity with EGFR inhibitors in cancer cells. Vps34-IN-5 is administered orally alone or with Erlotinib (HY-50896) in mouse xenograft models. Vps34-IN-5 can be used for the research of non-small cell lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 1801903-15-0
- Formula: C22H17ClF2N6O2S
- Molecular Weight:502.92
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Vps34-IN-5 (Ⅰ-299) exhibits additive anti-proliferative activity in combination with Erlotinib (HY-50896), Afatinib (HY-10261), AZD9291 (HY-15772), or CO-1686 (HY-15729) in A431 cells, with combination indices ranging from 1.00 to 1.02[1].
Vps34-IN-5 exhibits synergistic anti-proliferative activity in combination with afatinib, CO-1686, or erlotinib, and additive activity with AZD9291, in NCI H-1650 cells[1].
Vps34-IN-5 exhibits synergistic anti-proliferative activity in combination with afatinib or AZD9291, and additive activity with CO-1686, in NCI-H1975 cells[1].
Vps34-IN-5 exhibits additive anti-proliferative activity in combination with erlotinib, AZD9291, or CO-1686, and subadditive activity with afatinib, in PC9 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Vps34-IN-5 (0.65 mg/kg; p.o.; daily; 21 days) plus erlotinib (50/mg/kg) reduces tumor volume when used alone in nude female mice bearing human tumor xenografts[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude (female; inoculated subcutaneously in the flank with 2.0 × 106 tumor cells for tumor xenograft model)[1]
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Dosage:0.65 mg/kg; 0.65 mg/kg plus erlotinib (50/mg/kg)
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Administration:p.o.; daily; 21 days
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Result:Inhibited tumor growth when used alone.
Reduced tumor volume when used in combination with erlotinib.
Chemical Information
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CAS No. 1801903-15-0
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Molecular Weight 502.92
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Formula C22H17ClF2N6O2S
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SMILES
O=S(NC1=C(N=CC(C2=CC(NC3=NC(C)=NC=C3)=NC=C2)=C1C)Cl)(C4=CC=C(C=C4F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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